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异狄氏剂在兔体内的代谢归宿

The metabolic fate of endrin in the rabbit.

作者信息

Bedford C T, Harrod R K, Hoadley E C, Hutson D H

出版信息

Xenobiotica. 1975 Aug;5(8):485-500. doi: 10.3109/00498257509056119.

DOI:10.3109/00498257509056119
PMID:809931
Abstract
  1. [14C]Endrin, administered orally to rabbits, is excreted in the faeces as unchanged endrin (50% of that administered) and in the urine as a mixture of polar metabolites. 2. The major biotransformation is hydroxylation at the methylene bridge (C-12) to yield anti-12-hydroxyendrin. syn-Hydroxylation at C-12 also occurs. 3. The hydroxylated metabolites are excreted mainly as their sulphate conjugates. 4. Glucuronide conjugates are also excreted. anti-12-Hydroxyendrin is rapidly conjugated in vitro on incubation with rabbit liver microsomal glucuronyl transferase and UDPGA. 5. Comparative aspects of the metabolism of endrin in rats and rabbits are discussed.
摘要
  1. 给兔子口服[14C]异狄氏剂后,它以未变化的异狄氏剂形式(占给药量的50%)经粪便排泄,以极性代谢物混合物的形式经尿液排泄。2. 主要的生物转化是在亚甲基桥(C-12)处发生羟基化,生成反式-12-羟基异狄氏剂。C-12处也会发生顺式羟基化。3. 羟基化代谢物主要以其硫酸盐结合物的形式排泄。4. 葡糖醛酸结合物也会排泄。反式-12-羟基异狄氏剂在与兔肝微粒体葡糖醛酸基转移酶和UDPGA一起温育时,在体外会迅速结合。5. 讨论了大鼠和兔子体内异狄氏剂代谢的比较情况。

相似文献

1
The metabolic fate of endrin in the rabbit.异狄氏剂在兔体内的代谢归宿
Xenobiotica. 1975 Aug;5(8):485-500. doi: 10.3109/00498257509056119.
2
Detoxication and bioactivation of endrin in the rat.大鼠体内异狄氏剂的解毒作用与生物活化
Xenobiotica. 1975 Nov;5(11):697-714. doi: 10.3109/00498257509056139.
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Metabolism of labetalol by animals and man.拉贝洛尔在动物和人体内的代谢。
Br J Clin Pharmacol. 1976 Aug;3(4 Suppl 3):695-710.
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In vitro and in vivo metabolism of desogestrel in several species.去氧孕烯在几种物种中的体外和体内代谢。
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Carpipramine metabolism in the rat, rabbit and dog and in man after oral administration.口服给药后大鼠、兔、犬及人体中卡比咪嗪的代谢情况。
Xenobiotica. 1985 May;15(5):421-35. doi: 10.3109/00498258509045013.
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Elucidation of phase I and phase II metabolic pathways of rhein: species differences and their potential relevance.大黄酸Ⅰ相和Ⅱ相代谢途径的阐明:种属差异及其潜在相关性
Drug Metab Dispos. 1997 Apr;25(4):442-52.
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Metabolic fate of the thrombolytic agent benzarone in man: comparison with the rat and dog.溶栓剂苄佐那在人体内的代谢转归:与大鼠和犬的比较。
Xenobiotica. 1987 Jul;17(7):881-96. doi: 10.3109/00498258709043998.
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Species-dependent glucuronidation of drugs by immobilized rabbit, rhesus monkey, and human UDP-glucuronyltransferases.固定化兔、恒河猴和人尿苷二磷酸葡萄糖醛酸基转移酶对药物的种属依赖性葡萄糖醛酸化作用。
Drug Metab Dispos. 1987 Jul-Aug;15(4):473-7.
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Biotransformation of D(-)-ephedrine and L(+)-ephedrine in the rabbit, in vivo and in vitro.D(-)-麻黄碱和L(+)-麻黄碱在兔体内及体外的生物转化
Drug Metab Dispos. 1977 Jan-Feb;5(1):37-46.
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[Biotransformation of tramadol in man and animal (author's transl)].曲马多在人和动物体内的生物转化(作者译)
Arzneimittelforschung. 1981;31(11):1932-43.

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